Pilaralisib (XL147)

Catalog No.S7645

Pilaralisib (XL147) Chemical Structure

Molecular Weight(MW): 541.02

Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2.

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  • G, tumor growth response of HR6 tumors grown in athymic nude mice and treated with single and combination treatments. H, table of earliest detectable (P < 0.05) reduction in tumor size for control versus treated mice. ^, tumors that initially shrank and then grew; NS, not significant. I, OMI index initially decreases in HR6 organoids treated with paclitaxel, XL147, and combination therapies at 24 hours. J, OMI index of HR6 organoids treated for 72 hours. Red bars, significant reductions in OMI index; P< 0.05, for treated organoids versus control. Blue bars, significant increases in OMIindex;P< 0.05, for treated organoids versus control.

    Cancer Res, 2014, 74(18):5184-5194.. Pilaralisib (XL147) purchased from Selleck.

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Biological Activity

Description Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2.
Targets
PI3Kγ [1] PI3Kβ [1] PI3Kδ [1] PI3Kα [1]
23 nM 36 nM 36 nM 39 nM
In vitro

Pilaralisib exhibits cytotoxic activity in Pediatric Preclinical Testing Program (PPTP) cell lines, with a median relative IC50 value of 10.9 mM (range 2.7 mM to 24.5 mM).[2]

In vivo In BALB/c nu/nu mice, Pilaralisib (100 mg/kg, p.o.) induces tumor growth inhibition for solid glioma xenografts. Pilaralisib is well tolerated, with only 0.7% toxicity rate in the treated groups, similar to that observed for control animals.[2] In athymic female mouse, Pilaralisib (100 mg/kg, p.o.) significantly delays tumor growth without significant drug-related toxicity.[3]

Protocol

Kinase Assay: [4]
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In vitro kinase inhibition assays:

Kinase activity for PI3K isoforms is measured as the percentage of ATP consumed following the kinase reaction using luciferase–luciferin-coupled chemiluminescence, with ATP concentrations approximately equal to the Km for each respective kinase. Kinase reactions are initiated by combining test compounds, ATP and kinase in a 20 μL volume. PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ final enzyme concentrations are 0.5, 8, 20, and 2 nM, respectively. Of note, 0.5 μL dimethyl sulfoxide (DMSO) containing varying concentrations of the test compound is mixed with 10 μL enzyme solution (2×concentration). Kinase reactions are initiated by the addition of 10 μL of liver phosphatidylinositol and ATP solution (2×concentration). Assay concentrations for VPS34, ATP, and phosphatidylinositol are 40 nM, 1 μM, and 5 μM, respectively
Cell Research:[5]
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  • Cell lines: BT474 cells
  • Concentrations: 6 μM
  • Incubation Time: 5 days
  • Method: Cell proliferation is measured by using MTT or pre-mixed WST-1 reagent. For MTT/WST-1 assays, 10,000 cells/well are seeded in 96-well plates. 24 h after plating, cells are treated with DMSO or pilaralisib. After 5 days of treatment, MTT/WST-1 assays are performed.
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: BALB/c nu/nu mice with glioma xenografts
  • Formulation: 10 mM HCl in sterile water
  • Dosages: 100 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (184.83 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
10 mM HCl in sterile water
0.5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 541.02
Formula

C25H25ClN6O4S

CAS No. 934526-89-3
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01357330 Completed Solid Tumors Sanofi May 2011 Phase 1
NCT01240460 Completed Glioblastoma|Astrocytoma, Grade IV Sanofi January 2011 Phase 1
NCT01082068 Completed Breast Cancer Sanofi June 2010 Phase 1|Phase 2
NCT01042925 Completed Breast Cancer|Breast Neoplasms Sanofi February 2010 Phase 1|Phase 2
NCT01013324 Completed Endometrial Cancer|Endometrial Neoplasms Sanofi January 2010 Phase 2
NCT00756847 Completed Cancer|Non-Small Cell Lung Cancer|Endometrial Carcinoma|Ovarian Carcinoma Sanofi September 2008 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID